Inhibitors of Kinases and Phosphatases

Spotlight:

Acetylation and Methylation:Epigenetic Modulators of Gene Expression

The dynamic structural and functional scaffold of chromatin plays a vital role in many cellular processes, and is influenced by both genetic and epigenetic factors. DNA methylation and the post-translational modifications of histones are regarded as the major epigenetic factors.

Kinase Inhibitors

Small Molecule Inhibitors of Kinases

Protein kinases are enzymes that phosphorylate proteins on specific serine, threonine, or tyrosine residues. Stimulation of protein kinases is one of the most common mechanisms of signal transduction in cellular growth and differentiation. Protein kinases can be activated by calcium/calmodulin, phospholipids, cAMP and cGMP, growth factors, cytokines, and even toxins.

Small Molecule Inhibitors of Phosphatases

Protein Phosphatases modulate physiological responses by causing dephosphorylation of protein kinases and other proteins. They act on proteins involved in muscle contraction, protein synthesis, cholesterol metabolism, and several other biological processes. They can be inhibited by okadaic acid, calyculin, tautomycin, certain vanadium compounds, and other phosphatase inhibitors.

Small molecule inhibitors offer a powerful tool to assess the biological effects of perturbing signaling mediated by various protein kinases and phosphatases. Calbiochem® provides high quality small molecules that potently inhibit a broad-spectrum of protein kinases and phosphatases, which have been cited in numerous peer-reviewed publications. Explore our extensive collection below.

AKT (Protein Kinase B) Inhibitors

Akt, also known as protein kinase B (PKB), a serine/threonine kinase, is a critical enzyme in several signal transduction pathways involved in cell proliferation, apoptosis, angiogenesis, and diabetes. Four different isoforms of Akt (α, β1, β2, and γ) have been reported that differ slightly in the localization of their regulatory phosphorylation sites. Activation of Akt involves growth factor binding to a receptor tyrosine kinase and activation of PI 3-K, which phosphorylates the membrane bound PI(4,5)P2 (PIP2) to generate PI(3,4,5)P3 (PIP3) ...

MAP Kinase Inhibitors

The mitogen-activated protein (MAP) kinases are a group of evolutionarily conserved protein serine/threonine kinases that are activated in response to a variety of extracellular stimuli and mediate signal transduction from the cell surface to the nucleus. They regulate several physiological and pathological cellular phenomena, including inflammation, apoptotic cell death, oncogenic transformation, tumor cell invasion, and metastasis. MAP kinases, in combination with several other signaling pathways, can differentially alter the phosphorylation status of transcription factors in a pattern unique to a given external signal ...

Protein Phosphatase Inhibitors

Phosphorylation and dephosphorylation of structural and regulatory proteins are major intracellular control mechanisms in eukaryotes. Protein kinases transfer a phosphate from ATP to a specific protein, typically at serine, threonine, or tyrosine residues. Phosphatases remove the phosphoryl group and restore the protein to its original dephosphorylated state. Hence, the phosphorylation-dephosphorylation cycle can be regarded as a molecular "on-off" switch. Protein phosphatases (PPs) have been classified into three distinct categories: serine/threonine (Ser/Thr)-specific, tyrosine-specific, and dual-specificity phosphatases ...

Protein Tyrosine Kinase Inhibitors

Phosphorylation of tyrosine residues modulate enzymatic activity and create binding sites for recruitment of downstream signaling proteins. Protein tyrosine kinases (PTKs) play a key role in the regulation of cell proliferation, differentiation, metabolism, migration, and survival. They are classified as receptor PTKs and non-receptor PTKs. Selective receptor and non-receptor PTK inhibitors represent a promising class of anti-tumor agents. These agents are shown to inhibit multiple features of cancer cells, including proliferation, survival, invasion, and angiogenesis ...